Universal reference book for medicines
Product name: ISOPTIN ® (ISOPTIN ® )

Active substance: verapamil

Type: Calcium channel blocker

Manufacturer: ABBOTT (Germany) produced by EBEWE PHARMA (Austria)
Composition, form of production and packaging
The solution for intravenous administration is
clear, colorless.

1 amp.

verapamil hydrochloride 5 mg

Excipients: sodium chloride - 17 mg, hydrochloric acid 36% - until the pH is adjusted, water d / and - up to 2 ml.

2 ml - ampoules of colorless glass (5) - pallets (1) - packs of cardboard.

2 ml - ampoules of colorless glass (10) - pallets (1) - packs of cardboard.

2 ml - ampoules of colorless glass (50) - pallets (1) - packs of cardboard.

2 ml - ampoules of colorless glass (5) - blisters (1) - packs of cardboard.

2 ml - ampoules of colorless glass (10) - blisters (1) - packs of cardboard.

2 ml - ampoules of colorless glass (50) - blisters (1) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

Verapamil blocks transmembrannoe intake of calcium ions (and possibly sodium ions) in the cells of the conductive system of the myocardium and smooth muscle cells of the myocardium and vessels.
Antiarrhythmic action of verapamil is probably associated with its effect on slow channels in the cells of the conduction system of the heart.
The electrical activity of the sinoatrial and AV nodes is largely dependent on the entry of calcium into the cells through slow channels.
Inhibiting this intake of calcium, verapamil slows atrioventricular conduction and increases the effective refractory period in the AV node in proportion to heart rate. This effect leads to a decrease in the frequency of ventricular contractions in patients with atrial fibrillation and / or atrial flutter. By stopping the re-entry of excitation in the AV node, verapamil can restore the correct sinus rhythm in patients with paroxysmal supraventricular tachycardia, including Wolff-Parkinson-White syndrome (WPW).Verapamil does not interfere with conduction through additional conductive pathways.
Verapamil does not affect the unchanged atrial action potential and the time of intraventricular conduction, but lowers the amplitude, speed of depolarization and conduction in altered atrial fibers.

Verapamil does not cause spasm of the peripheral arteries and does not change the total content of calcium in the blood plasma.
Verapamil reduces postnagruzku and contractility of the myocardium. In most patients, including patients with organic heart lesions, the negative inotropic effect of verapamil is offset by a decrease in postload, the cardiac index usually does not change, but in patients with moderate and severe heart failure (pulmonary artery wedge pressure more than 20 mm Hg, ejection fraction less than 30%), there may be progression of circulatory failure. The maximum therapeutic effect is observed 3-5 minutes after the bolus IV injection of verapamil.
Usual doses of verapamil 5-10 mg with IV administration cause a transient, usually asymptomatic decrease in normal blood pressure, systemic vascular resistance and contractility, the filling pressure of the left ventricle slightly increases.

PHARMACOKINETICS

Verapamil hydrochloride for intravenous administration is rapidly metabolized.
The blood concentration change curve has a bi-exponential character with a fast early distribution phase (T 1/2 about 4 min), which is accompanied by a slower terminal elimination phase (T 1/2 2-5 h).
The connection with plasma proteins is about 90%.
The drug undergoes intensive metabolism with the formation of a large number of metabolites (when the drug is taken internally identified 12, most of which are found only in trace concentrations). Among metabolites, only noravapamil has a pharmacological effect (about 20% compared to the parent compound).
Verapamil hydrochloride and its metabolites are excreted by 70% kidneys (3-5% unchanged), 25% - with bile.
It is not excreted by hemodialysis.
Impaired renal function does not affect the pharmacokinetics of verapamil hydrochloride, as shown in comparative studies in patients with terminal renal insufficiency and healthy patients.

T 1/2 increases in patients with impaired hepatic function due to a decrease in metabolism during the first passage and an increase in the volume of distribution.

Verapamil penetrates through blood-brain and placental barriers, excreted in breast milk.

INDICATIONS

For the treatment of supraventricular tachyarrhythmias, namely:

- recovery of sinus rhythm in paroxysmal supraventricular tachycardia, including conditions associated with the presence of additional pathways (Wolff-Parkinson-White syndrome (WPW) and Louna-Ganong-Levin (LGL));

- control of the frequency of ventricular contractions in atrial flutter and atrial fibrillation (tachyarrhythmic variant), except when flutter or atrial fibrillation is associated with the presence of additional pathways (Wolff-Parkinson-White syndrome (WPW) and Louna-Ganong-Levin LGL)).

DOSING MODE

Only intravenously!

I / O administration should be done slowly for at least 2
min with continuous monitoring of ECG and blood pressure. In elderly patients, administration is carried out for at least 3 minutes to reduce the risk of unwanted effects.
The initial dose is 5-10 mg (0.075-0.15 mg / kg body weight).
A repeat dose of 10 mg (0.15 mg / kg body weight) is given 30 minutes after the first administration with an inadequate response to the first administration.
SIDE EFFECT

Most of the side effects listed below are most typical of isoptin tablets.

On the part of the cardiovascular system: reddening of the face, pronounced bradycardia, atrioventricular blockade, marked decrease in blood pressure, the appearance of symptoms of heart failure when using the drug in high doses, especially in predisposed patients;
stopping the sinus node, tachycardia, palpitations; rarely - angina pectoris up to the development of myocardial infarction (especially in patients with severe obstructive lesions of the coronary arteries), arrhythmia (including fibrillation and flutter of the ventricles), bradycardia.
On the part of the digestive system: nausea, vomiting, constipation, intestinal obstruction, a feeling of discomfort and abdominal pain: in some cases - a transient increase in the activity of hepatic transaminases and alkaline phosphatase in the blood plasma;
rarely - diarrhea, gingival hyperplasia (bleeding, soreness, swelling), increased appetite.
From the side of the nervous system: anxiety, general weakness, drowsiness, depression, extrapyramidal disorders (ataxia, masky face, shuffling gait, stiffness of hands or feet, trembling of hands and fingers, difficulty swallowing), dizziness, headache, convulsions during the injection of verapamil hydrochloride, paresthesia, tremor, in rare cases - increased nervous excitability, inhibition, fatigue.

Allergic reactions: skin rash, hyperemia of the facial skin, multiforme exudative erythema, Stevens-Johnson syndrome, itching, bronchospasm.

Other: weight gain;
very rarely - agranulocytosis, arthritis, transient blindness at the peak of the drug concentration in the blood, pulmonary edema, asymptomatic thrombocytopenia, development of peripheral edema, gynecomastia, hyperprolactinaemia, galactorrhea, impotence, increased sweating, muscle weakness, myalgia, joint pain, fatigue.
CONTRAINDICATIONS

- arterial hypotension or cardiogenic shock (except for caused by arrhythmia);

- AV blockade II and III degree (excluding patients with an artificial pacemaker);

- Morgagni-Adams-Stokes syndrome;

- syndrome of weakness of the sinus node (excluding patients with an artificial pacemaker);

- Sinoauric blockade;

- Wolff-Parkinson-White syndrome (WPW) and Louna-Ganong-Levin (LGL) combined with flutter or atrial fibrillation (except for patients with a pacemaker);

- ventricular tachycardia with wide QRS complexes (> 0.12 sec);

- Chronic heart failure of IIB-III stage (except for caused by supraventricular tachycardia, subject to treatment with verapamil);

- simultaneous use of beta-blockers (IV);

- preliminary (within 48 h) use of disopyramide;

- Pregnancy;

- lactation period;

- age under 18 years (effectiveness and safety not established);

- Hypersensitivity to the drug and its components.

With caution, the drug should be prescribed for AV blockade of the first degree, bradycardia, severe aortic stenosis, heart failure, mild or moderate arterial hypotension, myocardial infarction with left ventricular failure, hepatic and / or renal insufficiency, and in elderly patients.

PREGNANCY AND LACTATION

Contraindication: pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution, the drug should be prescribed for kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution, the drug should be prescribed for liver failure.

APPLICATION FOR CHILDREN

Contraindication: age under 18 years (efficacy and safety not established).

APPLICATION IN ELDERLY PATIENTS

In elderly patients, administration is carried out for at least 3 minutes to reduce the risk of unwanted effects.

SPECIAL INSTRUCTIONS

In / in the administration of isoptin often causes a transient reduction in blood pressure usually not manifested clinically, but which may be accompanied by dizziness.

Insufficiency of blood circulation (except for severe or caused by arrhythmia) should be compensated with cardiac glycosides and diuretics before the initiation of Isoptin therapy.
In patients with moderate and severe heart failure (pulmonary artery wedge pressure more than 20 mm Hg, ejection fraction less than 30%), with the administration of Isoptin, acute progression of circulatory failure can be observed.
The solution does not contain bacteriostatic or antimicrobial agents and is intended for simultaneous IV administration.

Verapamil hydrochloride remains stable for at least 24 hours at 25 ° C and protected from light in most parenteral solutions of large volume.
The remaining unused solution should be destroyed immediately after taking a portion of the contents of any volume.
To avoid disturbance of stability, it is recommended to dilute Isoptin with sodium lactate solutions in plastic bags of PVC.
It is necessary to avoid mixing solutions of Isoptin and albumin, amphotericin B, hydralazine hydrochloride or trimethoprim and sulfamethoxazole.
Verapamil hydrochloride precipitates in any solution with a pH greater than 6.

Impact on the ability to drive vehicles and manage mechanisms

Depending on the individual characteristics of the patient, isoptin can change the reaction rate, disrupting the ability to drive, work with machinery or in hazardous conditions.

OVERDOSE

Symptoms: sinus bradycardia, turning into atrioventricular blockade, sometimes asystole, marked decrease in blood pressure, heart failure, shock, sinoatrial blockade, hyperglycemia, metabolic acidosis.

Treatment: in case of rhythm and conduction disturbance - iv injection of isoprenaline, noradrenapine, 10-20 ml of 10% calcium gluconate solution, artificial pacemaker;
IV infusion of plasma-substituting solutions. Hemodialysis is not effective. To increase blood pressure in patients with hypertrophic cardiomyopathy, alpha-adrenostimulants (phenylephrine) are prescribed; Do not use isoprenaline and noradrenaline.
DRUG INTERACTION

Simultaneous administration of verapamil with drugs that reduce adrenergic activity can lead to excessive lowering of blood pressure.

Since verapamipa hydrochloride binds highly to plasma proteins, it must be used with caution at the same time as drugs that also bind highly to plasma proteins.

With the simultaneous use of verapamil hydrochloride with inhalational anesthetics, doses of drugs should be selected with caution in order to avoid excessive inhibition of the cardiovascular system.

With the simultaneous administration of verapamil hydrochloride with digoxin, careful monitoring of patients for the development of atrioventricular blockade or excessive bradycardia is necessary.

With the simultaneous use of verapamil with:

antiarrhythmic agents, beta-blockers and inhalation anesthetics, there is an increase in cardiotoxic effect (increased risk of atrioventricular blockade, a sharp decrease in heart rate, the development of heart failure, a sharp drop in blood pressure);

antihypertensive agents, diuretics, prazosin and other alpha-adrenoblockers - it is possible to strengthen the hypotensive effect of verapamil;

muscle relaxants - may enhance the muscle relaxant effect;

Acetylsalicylic acid - increased possibility of bleeding;

carbamazepine and lithium - the risk of neurotoxic effects increases;

quinidine - the level of concentration of quinidine in the blood plasma increases, the threat of lowering blood pressure increases, and in patients with hypertrophic cardiomyopathy, the emergence of severe arterial hypotension and pulmonary edema;

flecainide - it is possible to reduce the contractility of the myocardium, slow the atrioventricular conduction and prolong the repolarization period.

Dysopyramide should not be used within 48 hours before and 24 hours after using verapamil hydrochloride.

Procainamide, quinidine and other drugs that cause prolongation of the QT interval increase the risk of its significant lengthening.

Verapamil increases the concentration in the blood of digoxin, theophylline, prazosin, cyclosporine, carbamazepine, muscle relaxants, quinidine, valproic acid due to suppression of metabolism involving cytochrome P450.
It is possible to increase the concentration in the blood of midazolam, simvastatin, lovastatin, ethanol.
Rifampicin, barbiturates, nicotine, accelerating metabolism in the liver, lead to a decrease in the concentration of verapamil in the blood, reduce the severity of antianginal, hypotensive and antiarrhythmic actions.

NSAIDs reduce the hypotensive effect due to suppression of prostaglandin synthesis, sodium retention and fluid in the body.

Sympathomimetics reduce the hypotensive effect of verapamil.

Estrogens reduce the hypotensive effect due to fluid retention in the body.

Cimetidine has no effect on the pharmacokinetics of intravenous hydrochloride injected into verapamil.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in places inaccessible to children at a temperature of no higher than 25 ° C.
Shelf life - 5 years.
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